1. Epigenetics
  2. Histone Methyltransferase
  3. SGC0946

SGC0946 

Cat. No.: HY-15650 Purity: 99.68%
COA Handling Instructions

SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells.

For research use only. We do not sell to patients.

SGC0946 Chemical Structure

SGC0946 Chemical Structure

CAS No. : 1561178-17-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 108 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 108 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 79 In-stock
Estimated Time of Arrival: December 31
10 mg USD 139 In-stock
Estimated Time of Arrival: December 31
50 mg USD 554 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

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Description

SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells[1][2][3].

IC50 & Target

DOT1L

0.3 nM (IC50)

In Vitro

SGC0946 (0-100 µM; 4 days) inhibits DOT1L with IC50 of 2.65 nM in A431 cells[1].
SGC0946 (1, 5 µM; 14 days) displays selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells (transformed with the MLL-AF9 fusion oncogene)[1].
SGC0946 (1 µM; 3-7 days) shows time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation[1].
SGC0946 (1 µM, 7 days) effectively inhibits MLL target genes, HOXA9 and Meis1[1].
SGC0946 (0.2, 2, or 20 μM; 12 days) reduces proliferation and survival of ovarian cancer cells by inhibiting DOT1L enzymatic activity[2].
SGC0946 (10 μM; 12 days) induces G1 phase arrest by blocking DOT1L in SK-OV-3 and TOV21G cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A431 cells
Concentration: 0-100 µM
Incubation Time: 4 days
Result: Showed potent inhibitory activity against DOT1L with IC50 of 2.65 nM in A431 cells.

Cell Viability Assay[1]

Cell Line: Human cord blood cells (transformed with the MLL-AF9 fusion oncogene).
Concentration: 1, 5 µM
Incubation Time: 14 days
Result: Killed human cord blood cells transformed with an MLL-AF9 fusion oncogene.

Western Blot Analysis[1]

Cell Line: Molm13 MLL cells
Concentration: 1 µM
Incubation Time: 3-7 days
Result: Reduced H3K79me2 in Molm13 MLL cells in a time- and dose-dependent manner, and a complete inhibition exhibited at day 7.

Cell Proliferation Assay[2]

Cell Line: SK-OV-3 and TOV21G cells
Concentration: 0.2, 2, or 20 μM
Incubation Time: 12 days
Result: Inhibited the growth of both SK-OV-3 and TOV21G cells in a dose- and time-dependent manner.
Reduced the colony of both SK-OV-3 and TOV21G cells.

Cell Cycle Analysis[2]

Cell Line: SK-OV-3 and TOV21G cells
Concentration: 10 μM
Incubation Time: 12 days
Result: Induced increased G1 population and decreased S phase and G2/M phase cells in asynchronized SK-OV-3 and TOV21G cells.
In Vivo

SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD-SCID mice (4-week-old; mouse orthotopic xenograft ovarian cancer model)[2].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; twice a week for 6 weeks.
Result: Significantly suppressed growth of tumor (size and weight of tumor masses smaller than the untreated group).
Inhibited DOT1L enzymatic activity and decreased H3K79me2,CDK6, and cyclin D3 levels in the tumors.
Molecular Weight

618.57

Formula

C28H40BrN7O4

CAS No.
SMILES

NC1=NC=NC2=C1C(Br)=CN2[[email protected]]3[[email protected]](O)[[email protected]](O)[[email protected]@H](CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C)O3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (80.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6166 mL 8.0832 mL 16.1663 mL
5 mM 0.3233 mL 1.6166 mL 3.2333 mL
10 mM 0.1617 mL 0.8083 mL 1.6166 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.68%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SGC0946
Cat. No.:
HY-15650
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